JNJ-54175446 (C09-1140-875)

JNJ-54175446 is a potent and selective brain penetrant P2X7 receptor antagonist, with pIC 50 s of 8.46 and 8.81 for hP2X7 receptor and rP2X7 receptor, respectively.In VitroJNJ-54175446 (Compound 14) is a potent and selective brain penetrant P2X7 antagonist, with pIC 50 s of 8.46 and 8.81 for hP2X7 and rP2X7, respectively. JNJ-54175446 shows less potent activity against mouse, dog and Macaque P2X7 (pIC 50 , 7.8, 7.9 and 8.1, respectively). MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoJNJ-54175446 shows dose-dependent occupancy with the ED 50 of 0.46 mg/kg, corresponding to plasma EC 50 of 105 ng/mL . MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:pIC50: 8.46 (hP2X7 receptor), 8.81 (rP2X7 receptor). Specification: 0.99 Molecular Formula: C18H13ClF4N6O Molecular Weight: 440.78 PubChem CID: 90409366 Isomeric SMILES: C[C@@H]1C2=C(CCN1C(=O)C3=C(C(=CC=C3)C(F)(F)F)Cl)N(N=N2)C4=NC=C(C=N4)F